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Article

Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices.

Proceedings of the National Academy of Sciences of the United States of America - 10 Feb 2015

Leshchiner Elizaveta S, Parkhitko Andrey, Bird Gregory H, Luccarelli James, Bellairs Joseph A, Escudero Silvia, Opoku-Nsiah Kwadwo, Godes Marina, Perrimon Norbert, Walensky Loren D

Abstract excerpt

Activating mutations in the Kirsten rat sarcoma viral oncogene homolog (KRAS) underlie the pathogenesis and chemoresistance of ∼ 30% of all human tumors, yet the development of high-affinity inhibitors that target the broad range of KRAS mutants remains a formidable challenge. Here, we report the development and validation of stabilized alpha helices of son of sevenless 1 (SAH-SOS1) as prototype therapeutics that...

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Source

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Identifiers

PMID: 25624485
DOI: 10.1073/pnas.1413185112
PMCID: PMC4330742

Genes

KRAS
SOS1

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 4 Sept 2026.

Related research

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Research trail→

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Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices.PMID 25624485Read ↗

SOS1-inspired hydrocarbon-stapled peptide as a pan-Ras inhibitor.Semantic proximity Read ↗

Targeting Son of Sevenless 1: The pacemaker of KRAS.Semantic proximity Read ↗

Targeting cancer with small-molecule pan-KRAS degraders.Semantic proximity Read ↗

BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition.Semantic proximity Read ↗

Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations.Semantic proximity Read ↗

Multiple medicinal chemistry strategies of targeting KRAS: State-of-the art and future directions.Semantic proximity Read ↗

Small molecule Son of Sevenless 1 (SOS1) inhibitors: a review of the patent literature.Semantic proximity Read ↗

SOS1: tracking the evolving path from promising to actionable therapeutic target in RAS-dependent cancers.Semantic proximity Read ↗

Cereblon-based Bifunctional Degrader of SOS1, BTX-6654, Targets Multiple KRAS Mutations and Inhibits Tumor Growth.Semantic proximity Read ↗

Discovery of novel indazole derivatives as SOS1 agonists that activate KRAS signaling.Semantic proximity Read ↗

Discovery of a potent and orally available SOS1 inhibitor with antitumor efficacy in KRAS-mutant colorectal cancers.Semantic proximity Read ↗

Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia.Semantic proximity Read ↗

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